CM-675

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CM-675 (CM675) 是一种有效的 PDE5 和 I 类-HDAC 双重抑制剂，对 PDE5A/HDAC1 的 IC50 分别为 114/673 nM。

CM-675 (CM675) is a potent, dual PDE5 and classI-HDAC inhibitor with IC50 of 114/673 nM for PDE5A/HDAC1, respectively; displays >10-fold selectivity over HDAC6; induces significant cellular responses (AcH3K9 and pCREB) at low concentrations (26-100 nM) with little cytotoxicity; shows an adequate ADME-Tox profile and in vivo target engagement (histone acetylation and cAMP/cGMP response element-binding (CREB) phosphorylation) in the central nervous system (CNS).

CM-675 (29a) shows a significant time-dependent effect on class I HDAC inhibition, particularly towards HDAC2. For HDAC1, its inhibitory potency also increased significantly (~1 log unit) with the pre-incubation time: 673 nM (30 min), 180 nM (4 hours) and 69 nM (6 hours) .

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CM675 | CM 675

Cell Cycle/DNA Damage

HDAC

HDAC

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1872466-47-1

536.636

C31H32N6O3

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (46.59 mM)

CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)CC4=CC=C(C=C4)C(=O)NC5=CC=CC=C5N)OCC)C

N-(2-aminophenyl)-4-[[4-ethoxy-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]methyl]benzamide

(-20℃)

With Ice Pack

≥ 2 years